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Assay Detail

CHEMBL682032

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity for Farnesoid X Receptor (FXR)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Bile acid receptor (CHEMBL2047)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Binding mode of 6ECDCA, a potent bile acid agonist of the farnesoid X receptor (FXR).
Costantino G, Macchiarulo A, Entrena-Guadix A, Camaioni E, Pellicciari R.
Bioorg Med Chem Lett (2003) 13 : 1865 -1868
PubMed 12749886 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 5.86 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL566315 OBETICHOLIC ACID 4.0 1 7.00
CHEMBL3137829 1 6.12
CHEMBL3138184 1 5.96
CHEMBL1552 GLYCOCHENODEOXYCHOLATE 1 5.52
CHEMBL185878 TAUROCHENODEOXYCHOLATE 1 5.52
CHEMBL240597 CHENODIOL 4.0 1 5.06
CHEMBL3137828 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL566315 OBETICHOLIC ACID EC50 = 99.0 nM 7.00
CHEMBL3137829 EC50 = 750.0 nM 6.12
CHEMBL3138184 EC50 = 1110.0 nM 5.96
CHEMBL1552 GLYCOCHENODEOXYCHOLATE EC50 = 3000.0 nM 5.52
CHEMBL185878 TAUROCHENODEOXYCHOLATE EC50 = 3000.0 nM 5.52
CHEMBL240597 CHENODIOL EC50 = 8660.0 nM 5.06
CHEMBL3137828 EC50 > 30000.0 nM -